2024-03-19T02:16:50Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/1541082021-12-27T16:54:11Zcom_10261_38com_10261_5col_10261_291
00925njm 22002777a 4500
dc
Varan, Gamze
author
Benito, Juan M.
author
Ortiz-Mellet, Carmen
author
Bilensoy, Erem
author
2017
Background: Paclitaxel is a potent anticancer drug that is effective against a wide spectrum of cancers. To overcome its bioavailability
problems arising from very poor aqueous solubility and tendency to recrystallize upon dilution, paclitaxel is commercially
formulated with co-solvents such as Cremophor EL® that are known to cause serious side effects during chemotherapy. Amphiphilic
cyclodextrins are favored oligosaccharides as drug delivery systems for anticancer drugs, having the ability to spontaneously
form nanoparticles without surfactant or co-solvents. In the past few years, polycationic, amphiphilic cyclodextrins were introduced
as effective agents for gene delivery in the form of nanoplexes. In this study, the potential of polycationic, amphiphilic cyclodextrin
nanoparticles were evaluated in comparison to non-ionic amphiphilic cyclodextrins and core–shell type cyclodextrin nanoparticles
for paclitaxel delivery to breast tumors. Pre-formulation studies were used as a basis for selecting the suitable organic solvent
and surfactant concentration for the novel polycationic cyclodextrin nanoparticles. The nanoparticles were then extensively
characterized with particle size distribution, polydispersity index, zeta potential, drug loading capacity, in vitro release profiles and
cytotoxicity studies.
Results: Paclitaxel-loaded cyclodextrin nanoparticles were obtained in the diameter range of 80−125 nm (depending on the nature
of the cyclodextrin derivative) where the smallest diameter nanoparticles were obtained with polycationic (PC) βCDC6. A strong
positive charge also helped to increase the loading capacity of the nanoparticles with paclitaxel up to 60%. Interestingly, cyclodextrin
nanoparticles were able to stabilize paclitaxel in aqueous solution for 30 days. All blank cyclodextrin nanoparticles were
demonstrated to be non-cytotoxic against L929 mouse fibroblast cell line. In addition, paclitaxel-loaded nanoparticles have a significant
anticancer effect against MCF-7 human breast cancer cell line as compared with a paclitaxel solution in DMSO.Conclusion: According to the results of this study, both amphiphilic cyclodextrin derivatives provide suitable nanometer-sized
drug delivery systems for safe and efficient intravenous paclitaxel delivery for chemotherapy. In the light of these studies, it can be
said that amphiphilic cyclodextrin nanoparticles of different surface charge can be considered as a promising alternative for selfassembled
nanometer-sized drug carrier systems for safe and efficient chemotherapy
Beilstein Journal of Nanotechnology, 8, 1457–1468 (2017)
http://hdl.handle.net/10261/154108
10.3762/bjnano.8.145
28900599
Amphiphilic cyclodextrin;
Anticancer
Nanoparticle
Paclitaxel
Polycationic
Development of polycationic amphiphilic cyclodextrin nanoparticles for anticancer drug delivery